The formal name of Docetaxel trihydrate is (2′R,3′S)-N-carboxy-3-phenylisoserine, N-tert-butyl ester, 13-ester with 5β,20-epoxy-1β,2α,4α,7β,10β,13α-hexahydroxytax-11-en-9-one 4-acetate-2-benzoate, trihydrate.
Docetaxel is a kind of new anti-cancer medicine that is being developed abroad in recent years. Being the representative of the 2nd generation of taxane medicine family, Docetaxel attracts more and more attention from people for its enhanced water-solubility and wide spectrum of excellent anti-cancer characteristic. Docetaxel has activity against several kinds of cancer, including breast cancer, non small cell lung cancer and other malignant tumours (prostate cancer, esophagus cancer and malignant tumour in head or neck, etc.), which is one of the most effective single medicine for treating the transferring breast cancer. The especially remarkable result of it is: in phase II clinical trial, for those patients who have received any chemotherapy (including those patient with primary resistence against anthracene, the total chemotherapy efficiency of single Docetaxel was 47% (generally 100 mgs/m2, infusion, once per 3 weeks). A few research reports showed that the efficiency of this drug is between 32% and 58%, among which one research reported CR (Complete Resultful) at 4%. For patients in the later-stage of none small cell lung cancer, no matter he/she was in the beginning of treatment, or has passed the progress of cis-platinum chemotherapy, the medicine proved its special anti-cancer activity.
Docetaxel can promote microtubule proteins to be assembled into microtubule and inhibit its disassembled. Docetaxel also has the good bioavailability, higher intracellular concentration and longer intracellular retention-time.
Docetaxel is the first semi-synthesized taxus medicine. It has been launched in the markets of Europe/America countries.
According to Chinese patent 95193984.X, Docetaxel trihydrate is more stable than its anhydrous compound. So we decided to add a crystallization process into the production procedure of the drug production. Ethanol and water are selected as solvents. But in this experiment process, the inventor discovered that use of the ethanol produces not only more time expense for concentration and higher water bath temperature, but also smaller crystal grain, thus longer time to filter and collect products is needed.